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目的:测定川芎和黄芪合用后川芎主要有效成分藁本内酯在心肌缺血大鼠体内的血药浓度及药代动力学参数。方法:舌下静脉给予3.5 mg.kg-1盐酸异丙肾上腺素诱发心肌缺血,于给药后不同时间点眼眶(眼球后静脉丛)采血1 mL,HPLC/MS法测定血浆藁本内酯含量,Win Nonlin计算药代动力学参数。结果:川芎-黄芪合用川芎的主要有效成分藁本内酯的药动学参数为:Cmax(0.737±0.181)mg·L-1;AUC(0-t)(75.20±10.35)mg·L-1·min-1;AUC(0-∞)(81.66±21.01)mg·L-1·min-1;MRT(0-t)(85.87±5.03)min;CL(0.0512±0.0118)L·min-1;t1/2(77.97±5.75)min;Vz(5.808±1.641)L·kg-1。结论:与川芎单用相比,黄芪-川芎合用后藁本内酯的AUC(0-t)显著增加,MRT(0-t)延长,说明两药配伍有利于提高藁本内酯的血药浓度及体内滞留,进而发挥其药理作用。
OBJECTIVE: To determine the plasma concentrations and pharmacokinetic parameters of ligustilide, a major active ingredient of ligusticum chuanxiong in rats with myocardial ischemia, after the combination of Chuanxiong and Astragalus. Methods: Myocardial ischemia was induced by intravenous injection of isoprenaline hydrochloride (3.5 mg.kg-1). One mL of blood was collected from the orbit (retropancreatic venous plexus) at different time points after administration. The contents of plasma ligustilide Content, Win Nonlin Calculate Pharmacokinetic Parameters. Results: The pharmacokinetic parameters of ligustilide were as follows: Cmax (0.737 ± 0.181) mg · L-1; AUC (0-t) (75.20 ± 10.35) mg · L-1 (0-t) (85.87 ± 5.03) min; CL (0.0512 ± 0.0118) L · min-1 ; t1 / 2 (77.97 ± 5.75) min; Vz (5.808 ± 1.641) L · kg-1. CONCLUSION: Compared with Ligusticum chuanxiong, the AUC (0-t) of ligustilide increased significantly and the MRT (0-t) prolonged after the combination of Astragalus and Ligusticum chuanxiong, indicating that the combination of two drugs is beneficial to increase the blood pressure of ligustilide Concentration and in vivo retention, and then play its pharmacological effects.